| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C24H28N4O3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
AZ31 is a potent, highly selective, orally active ATM inhibitor, with an IC50 below 1.2 nM against the ATM enzyme and an IC50 of 46 nM in cells. It shows excellent selectivity over ATR (>500-fold) as well as excellent selectivity across the PIKK family and the wider kinase panel. AZ31 is a potent radiosensitizer in vitro and can be used for cancer research[1]. It is supplied as an off-white to light yellow solid (C24H28N4O3, MW 420.50) at 99.21% purity.
Physical & Chemical Properties
| CAS Number | 2088113-98-6 |
|---|---|
| Molecular Formula | C24H28N4O3 |
| Molecular Weight | 420.50 g/mol |
| Purity | 99.21% |
| Appearance | Solid |
| Color | Off-white to light yellow |
| SMILES | O=C(C1=C(N[C@@H](C)C2CCOCC2)C3=CC(C4=CC=C(COC)N=C4)=CC=C3N=C1)N |
| Target | ATM |
| Signaling Pathway | Cell Cycle/DNA Damage; PI3K/Akt/mTOR |
| Solubility | In Vitro: DMSO: 100 mg/mL (237.81 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | -20°C, protect from light. In solvent: -80°C, 6 months; -20°C, 1 month (protect from light). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
ATM 1.2 nM (IC50) |
ATM 46 nM (IC50, in cell) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (237.81 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); protect from light; avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
AZ31 (0.3-3 μM; 1 h) alters phosphorylation across a panel of ATM targets[1]. In H2228 lung cancer cells after radiation, AZ31 (10 μM; 1 h) alters p53 stabilization[1].
Western Blot Analysis[1]
| Cell Line | Human glioma cell line |
|---|---|
| Concentration | 0.3, 1 and 3 μM |
| Incubation Time | 1 hour |
| Result | Blocked phosphorylation of p53-S15, KAP1-S824, and ATM auto-phosphorylation at S1981. |
Western Blot Analysis[1]
| Cell Line | H460 and mutant p53 H2228 cell lines |
|---|---|
| Concentration | 10 μM |
| Incubation Time | 1 hour |
| Result | Destabilized p53 of mutant p53 but not wild-type after radiation. |
In Vivo
Low brain coverage is seen with AZ31 (50-100 mg/kg; p.o. twice a day)[1].
| Animal Model | Nude mice[1] |
|---|---|
| Dosage | 50 and 100 mg/kg |
| Administration | Oral gavage; 50 and 100 mg/kg twice a day |
| Result | Exhibited exposure over IC50 at 0.046 μM in brain only for 2-3 hours. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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